2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK MAPK/ERK Pathway Stem Cell/Wnt Cell Cycle/DNA Damage Apoptosis
  3. EGFR ERK DNA/RNA Synthesis Apoptosis
  4. Len-604

Len-604 是一种 FGFR 抑制剂，对 FGFR4、FGFR1、FGFR2 和 FGFR3 的 IC50 分别为 9.71 nM、9.93 nM、29.80 nM 和 14.48 nM。Len-604 可下调 FGFR4 和 ERK 的磷酸化水平，可引发癌细胞 DNA 损伤和细胞凋亡 (apoptosis)。Len-604 可用于肝癌的相关研究。

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Len-604

Len-604 Chemical Structure

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Len-604 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

查看所有亚型
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

查看 DNA/RNA Synthesis 亚型特异性产品:

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Len-604 is a FGFR inhibitor with IC50 values of 9.71 nM, 9.93 nM, 29.80 nM and 14.48 nM against FGFR4, FGFR1, FGFR2 and FGFR3, respectively. Len-604 reduces the phosphorylation levels of FGFR4 and ERK, and induces DNA damage and apoptosis in cancer cells. Len-604 is applicable to research related to liver cancer[1].

IC50 & Target[1]

ERK1

 

ERK2

 

体外研究
(In Vitro)

Len-604 (72 h) 对 HUH-7 和 SMMC-7721 人肝癌细胞表现出强细胞毒性 (IC50 分别为 5.62 μM 和 5.64 μM)，且对非癌性 L02 肝细胞具有高选择性[1]。
Len-604 (10-30 μM; 24 h) 可在人肝癌细胞 HUH-7 中诱导剂量依赖性凋亡，30 μM 作用 24 h 后的凋亡率达 51.1%[1]。
Len-604 (10 μM; 24 h) 可在孵育 24 h 后诱导人肝癌细胞 HUH-7 发生 S 期细胞周期阻滞[1]。
Len-604 (10-20 μM; 24 h) 以剂量依赖方式下调人肝癌细胞 HUH-7 中 p-FGFR4 和 p-ERK1/2 的水平，且不改变总 FGFR4 和 ERK1/2 的蛋白水平[1]。
Len-604 (10 μM; 12-24 h) 可在人肝癌细胞 HUH-7 中诱导显著的 DNA 损伤，γ-H2AX 表达水平升高以及彗星实验检测到的 DNA 链断裂可证明这一点[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Len-604 相关抗体:

Apoptosis Analysis[1]

Cell Line: HUH-7
Concentration: 10, 20 and 30 μM
Incubation Time: 24 h
Result: Induced cell apoptosis in a dose-dependent manner.
At 10 μM, showed an apoptotic ratio higher than lenvatinib but lower than cisplatin and the lenvatinib-cisplatin mixture.
At 30 μM, reached an apoptotic ratio of 51.1%.

Cell Cycle Analysis[1]

Cell Line: HUH-7
Concentration: 10 μM
Incubation Time: 24 h
Result: Decreased G0-G1 phase cell distribution from 77.7% to 67.5% compared to control.
Increased S-phase distribution from 15.7% to 30.7% compared to control.
Caused S-phase arrest similar to cisplatin and the lenvatinib-cisplatin mixture.

Western Blot Analysis[1]

Cell Line: HUH-7
Concentration: 10 and 20 μM
Incubation Time: 24 h
Result: Downregulated phosphorylated FGFR4 (p-FGFR4) in a dose-dependent manner.
Downregulated phosphorylated ERK1/2 (p-ERK1/2) in a dose-dependent manner.
Left levels of total FGFR4 and ERK1/2 unchanged.
At 10 μM, showed inhibition of p-FGFR4 nearly equivalent to lenvatinib.
体内研究
(In Vivo)

Len-604 (5.0 mg/kg；静脉注射；每周 1 次；共 14 天) 在 HUH-7 异种移植小鼠中实现 61.25% 的肿瘤生长抑制率，且未观察到体重下降[1]。
Len-604 (15-25 mg/kg；静脉注射；每周 1 次；持续 21 天) 在 HUH-7 异种移植小鼠中分别实现了 64.96% 和 91.98% 的肿瘤生长抑制率，且全身毒性较低，同时可剂量依赖性地抑制 FGFR4/ERK 信号通路[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude (female, 6 weeks old, 16−18 g, HUH-7 hepatocellular carcinoma xenograft)[1]
Dosage: 5.0 mg/kg
Administration: i.v.; once weekly; 14 days
Result: Achieved a tumor growth inhibition (TGI) rate of 61.25%.
Showed no significant mouse weight loss, indicating low systemic toxicity.
Animal Model: BALB/c nude (female, 6 weeks old, 16−18 g, HUH-7 hepatocellular carcinoma xenograft)[1]
Dosage: 15.0 mg/kg; 25.0 mg/kg
Administration: i.v.; once weekly; 21 days
Result: Achieved a tumor growth inhibition (TGI) rate of 64.96% at 15.0 mg/kg.
Achieved a tumor growth inhibition (TGI) rate of 91.98% at 25.0 mg/kg.
Showed no significant changes in mouse body weight at both doses.
Revealed no toxic impacts on major organs (heart, liver, spleen, lung, kidney) via histopathological analysis.
Showed severe tumor cell degeneration/necrosis in tumor tissue sections.
Induced dose-dependent downregulation of phosphorylated FGFR4 (p-FGFR4) and phosphorylated ERK1/2 (p-ERK1/2) levels in tumor tissues via Western blot analysis.
分子量

880.17

Formula

C30H33ClN8O9Pt
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Len-604 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Len-604Len604Len 604EGFRERKDNA/RNA SynthesisApoptosisEpidermal growth factor receptorErbB-1HER1Extracellular signal regulated kinasesFGFR1ERK phosphorylationFGFR3human hepatocellular carcinoma cell linesFGFR2HUH-7SMMC-7721L02DNA damageFGFR4Inhibitorinhibitorinhibit

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